Amrubicin (hydrochloride)

Amrubicin (SM-5887) hydrochloride is a DNA topoisomerase II inhibitor, used for the research of cancer. IC50 & Target:Topoisomerase II^[1] In Vitro:Amrubicin (SM-5887) (2.5 μg/mL) shows radio-enhancement effects on human lung adenocarcinoma A549 cells^[1]. Amrubicin (SM-5887) supresses the LX-1, A549, A431, and BT-474 cell lines, with IC₅₀s of 1.1 ± 0.2, 2.4 ± 0.8, 0.61 ± 0.10 and 3.0 ± 0.3 µg/mL, respectively^[2]. Amrubicin (SM-5887) inhibits the cell cycle profile of U937 cells with an IC₅₀ of 5.6 µM. Amrubicin (20 µM) also induces apoptosis in U937 cells, activates caspase-3/7 and reduces the mitochondrial membrane potential (Δψm)^[3]. In Vivo:Amrubicin (SM-5887) (25 mg/kg, i.v.) exhibits significant antitumor activities against both SCLC tumors, Lu-24 and Lu-134, with T/C-values (comparing the mean tumor growth rates of the treated group with those of the control group for each day that the tumors are measured) at day 14 of 17% and 9%, respectively. Amrubicin (SM-5887) (25 mg/kg, i.v.) in combination with cisplatin and irinotecan significantly inhibits the growth of tumors compared to amrubicin alone in mice bearing LX-1 tumor cells. Amrubicin (SM-5887) alone or combined with tegafur and uracil also suppresses tumor growth in human cancer xenograft models^[2].